AR079328A1 - DERIVATIVES OF 9H-PIRIDINO [3,4-B] INDOL DISPOSED, METHOD TO PREPARE THEM, SYNTHESIS INTERMEDIARIES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND USE OF THE SAME IN CANCER THERAPY. - Google Patents

DERIVATIVES OF 9H-PIRIDINO [3,4-B] INDOL DISPOSED, METHOD TO PREPARE THEM, SYNTHESIS INTERMEDIARIES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND USE OF THE SAME IN CANCER THERAPY.

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Publication number
AR079328A1
AR079328A1 ARP100104536A ARP100104536A AR079328A1 AR 079328 A1 AR079328 A1 AR 079328A1 AR P100104536 A ARP100104536 A AR P100104536A AR P100104536 A ARP100104536 A AR P100104536A AR 079328 A1 AR079328 A1 AR 079328A1
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AR
Argentina
Prior art keywords
optionally mono
trisubstituted
alkyl
heteroaryl
branched
Prior art date
Application number
ARP100104536A
Other languages
Spanish (es)
Inventor
Alexandre Gross
Serge Mignani
Didier Babin
Olivier Bedel
Thierry Gouyon
Original Assignee
Sanofi Aventis
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Sanofi Aventis filed Critical Sanofi Aventis
Publication of AR079328A1 publication Critical patent/AR079328A1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Reivindicacion 1: Productos de la formula general (1) en la que Z3 representa un radical heteroarilo constituido por 5 o 6 miembros con 1 a 4 heteroátomos elegidos entre N, S u O asociado al resto carbonilo o por un C o por un N perteneciente a Z3, estando Z3 opcionalmente mono o polisustituido; Z6 se elige entre i) H, ii) halogeno, iii) -OH, iv) alcoxi cuya parte alquilo está opcionalmente mono, di o trisustituida; v) -Y-alquilo (Y = S, SO, SO2) lineal o ramificado, opcionalmente mono, di o trisustituido; vi) -X-arilo (X = O, S, SO, SO2) opcionalmente mono, di o trisustituido, vii) -X-heteroarilo (X = O, S, SO, SO2, heteroarilo de 5 o 6 miembros con 1 a 4 heteroátomos elegidos entre N, S u O asociado a X o por un C o por un N) opcionalmente mono, di o trisustituido; viii) NH2, ix) -NH(alquilo), -N(alquilo)2 lineal(es), ramificado(s) o cíclico(s) cuya parte alquilo está opcionalmente mono, di o trisustituida; x) -NH(arilo) cuya parte arilo está opcional mente mono, di o trisustituida; xi) -NH(heteroarilo) cuya parte heteroarilo (heteroarilo de 5 o 6 miembros con 1 a 4 heteroátomos elegidos entre N, S u O asociado al átomo de nitrogeno o por un C o por un N) está opcionalmente mono, di o trisustituida; xii) -N(alquil)(arilo) cuyas partes alquilo (lineal, ramificado o cíclico) y arilo están opcionalmente mono, di o trisustituidas; xiii) -N(alquil) (heteroarilo) cuyas partes alquilo (lineal, ramificado o cíclico) y heteroarilo (heteroarilo de 5 o 6 miembros con 1 a 4 heteroátomos elegidos entre N, S u O asociado al átomo de nitrogeno o por un C o por un N) están opcionalmente mono, di o trisustituidas; xiv) -C(O)OH, xv) -C(O)Oalquilo lineal, ramificado o cíclico, opcionalmente mono, di o trisustituido; xvi) -C(O)Oarilo opcionalmente mono, di o trisustituido; xvii) -C(O)Oheteroarilo (heteroarilo de 5 o 6 miembros con 1 a 4 heteroátomos elegidos entre N, S u O asociado al oxígeno por un átomo de C) opcionalmente mono, di o trisustituido; xviii) -CONH2, xix) -CO-heterocicloalquilo mono, di o trisustituido, xx) -CONH(alquilo), CON(alquilo)2 lineal(es), ramificado(s) o cíclico(s) cuya parte alquilo está opcionalmente mono, di o trisustituida; xxi) CON(alquil)(arilo), alquilo lineal, ramificado o cíclico, cuyas partes alquilo y arilo están opcionalmente mono, di o trisustituidas; xxii) -CON(alquil)(heteroarilo), alquilo lineal, ramificado o cíclico y heteroarilo de 5 o 6 miembros con 1 a 4 heteroátomos elegidos entre N, S u O asociado al átomo de nitrogeno o por un C o por un N) cuyas partes alquilo y heteroarilo están opcionalmente mono, di o trisustituidas; xxiii) -alquilo C1-10 lineal, ramificado o cíclico, que consta opcionalmente de un heteroátomo y está opcionalmente mono, di o trisustituido; xxiv) arilo opcionalmente mono, di o trisustituido; xxv) heteroarilo (5 o 6 miembros con 1 a 4 heteroátomos elegidos entre N, S u O) asociado al resto carbonilo o por un C o por un N perteneciente a Z6, estando Z6 opcionalmente mono o polisustituido; xxvi) heterocicloalquilo opcionalmente mono o polisustituido; xxvii) alquenilo C2-6 opcionalmente mono o disustituido; xxviii) -alquinilo C2-6 opcionalmente sustituido; estando dichos productos de la formula (1) en todas las formas posibles de isomeros, racémicos, enantiomeros y diastereoisomeros, así como las sales de adicion, con los ácidos minerales y orgánicos o con las bases minerales y orgánicas, de dichos productos de la formula (1).Claim 1: Products of the general formula (1) in which Z3 represents a heteroaryl radical consisting of 5 or 6 members with 1 to 4 heteroatoms chosen from N, S or O associated with the carbonyl moiety or by a C or an N belonging to Z3, Z3 being optionally mono or polysubstituted; Z6 is selected from i) H, ii) halogen, iii) -OH, iv) alkoxy whose alkyl part is optionally mono, di or trisubstituted; v) -Y-alkyl (Y = S, SO, SO2) linear or branched, optionally mono, di or trisubstituted; vi) -X-aryl (X = O, S, SO, SO2) optionally mono, di or trisubstituted, vii) -X-heteroaryl (X = O, S, SO, SO2, 5- or 6-membered heteroaryl with 1 to 4 heteroatoms chosen from N, S or O associated with X or by a C or by an optionally mono, di or trisubstituted N); viii) NH2, ix) -NH (alkyl), -N (linear), branched (s) or cyclic (N) alkyl whose alkyl part is optionally mono, di or trisubstituted; x) -NH (aryl) whose aryl part is optionally mono, di or trisubstituted; xi) -NH (heteroaryl) whose heteroaryl part (5- or 6-membered heteroaryl with 1 to 4 heteroatoms chosen from N, S or O associated with the nitrogen atom or by a C or by an N) is optionally mono, di or trisubstituted ; xii) -N (alkyl) (aryl) whose alkyl (linear, branched or cyclic) and aryl parts are optionally mono, di or trisubstituted; xiii) -N (alkyl) (heteroaryl) whose alkyl (linear, branched or cyclic) and heteroaryl (5- or 6-membered heteroaryl with 1 to 4 heteroatoms chosen from N, S or O associated with the nitrogen atom or by a C or by an N) are optionally mono, di or trisubstituted; xiv) -C (O) OH, xv) -C (O) Linear, branched or cyclic alkyl, optionally mono, di or trisubstituted; xvi) -C (O) Optionally mono, di or trisubstituted oaryl; xvii) -C (O) Oheteroaryl (5- or 6-membered heteroaryl with 1 to 4 heteroatoms chosen from N, S or O associated with oxygen by a C atom) optionally mono, di or trisubstituted; xviii) -CONH2, xix) -CO, mono, di or trisubstituted, heteroxycycloalkyl, xx) -CONH (alkyl), CON (linear) CON (alkyl) 2, branched (s) or cyclic (s) whose alkyl part is optionally mono , di or trisubstituted; xxi) CON (alkyl) (aryl), linear, branched or cyclic alkyl, whose alkyl and aryl parts are optionally mono, di or trisubstituted; xxii) -CON (alkyl) (heteroaryl), linear, branched or cyclic alkyl and 5- or 6-membered heteroaryl with 1 to 4 heteroatoms chosen from N, S or O associated with the nitrogen atom or by a C or by an N) whose alkyl and heteroaryl parts are optionally mono, di or trisubstituted; xxiii) - linear, branched or cyclic C1-10 alkyl, optionally consisting of a heteroatom and optionally mono, di or trisubstituted; xxiv) optionally mono, di or trisubstituted aryl; xxv) heteroaryl (5 or 6 members with 1 to 4 heteroatoms chosen from N, S or O) associated with the carbonyl moiety or by a C or by an N belonging to Z6, Z6 being optionally mono or polysubstituted; xxvi) optionally mono or polysubstituted heterocycloalkyl; xxvii) optionally mono or disubstituted C2-6 alkenyl; xxviii) -C2-6 alkynyl optionally substituted; said products of the formula (1) being in all possible forms of isomers, racemic, enantiomers and diastereoisomers, as well as the addition salts, with the mineral and organic acids or with the mineral and organic bases, of said products of the formula (one).

ARP100104536A 2009-12-10 2010-12-09 DERIVATIVES OF 9H-PIRIDINO [3,4-B] INDOL DISPOSED, METHOD TO PREPARE THEM, SYNTHESIS INTERMEDIARIES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND USE OF THE SAME IN CANCER THERAPY. AR079328A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
FR0958830A FR2953837B1 (en) 2009-12-10 2009-12-10 DISUBSTITUTED 9H-PYRIDINO [3,4-B] INDOLE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC USE

Publications (1)

Publication Number Publication Date
AR079328A1 true AR079328A1 (en) 2012-01-18

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ARP100104536A AR079328A1 (en) 2009-12-10 2010-12-09 DERIVATIVES OF 9H-PIRIDINO [3,4-B] INDOL DISPOSED, METHOD TO PREPARE THEM, SYNTHESIS INTERMEDIARIES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND USE OF THE SAME IN CANCER THERAPY.

Country Status (5)

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AR (1) AR079328A1 (en)
FR (1) FR2953837B1 (en)
TW (1) TW201130833A (en)
UY (1) UY33099A (en)
WO (1) WO2011070298A1 (en)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JO3407B1 (en) 2012-05-31 2019-10-20 Eisai R&D Man Co Ltd Tetrahydropyrazolopyrimidine Compounds
CN106588918B (en) * 2016-12-08 2019-02-19 广东省测试分析研究所（中国广州分析测试中心） A kind of preparation method and applications of 3- amino-beta-carboline
EP3860996A4 (en) 2018-10-02 2022-08-31 Northwestern University Beta-carbolines as positive allosteric modulators of the human serotonin receptor 2c (5-ht2c)

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JPS57123180A (en) * 1980-12-17 1982-07-31 Schering Ag 3-substituted beta-carboline, manufacture and psychotropic drug containing same
DK240084D0 (en) * 1984-05-15 1984-05-15 Ferrosan As NEW BETA-CARBOLINE-3-OXADIAZOLYL DERIVATIVES
DE3540653A1 (en) * 1985-11-13 1987-05-14 Schering Ag NEW 3-OXADIAZOLE AND 3-CARBONIC ACID SS-CARBOLINE DERIVATIVES, THEIR PRODUCTION AND THEIR USE AS MEDICINAL PRODUCTS
AU619203B2 (en) * 1987-08-28 1992-01-23 Schering Aktiengesellschaft Isoxazole-beta-carboline derivatives
US5502194A (en) 1992-02-19 1996-03-26 Bayer Aktiengesellschaft Process for the preparation of 2-halogeno-pyridine derivatives
DE4233708A1 (en) 1992-10-07 1994-04-14 Ruetgerswerke Ag Process for the preparation of pure 2,5-dichloropyridine and recovery of the 2,3-dichloropyridine obtained as a by-product
WO1996034865A1 (en) * 1995-05-05 1996-11-07 Novo Nordisk A/S Novel heterocyclic chemistry
WO2000063209A1 (en) * 1999-04-20 2000-10-26 Novo Nordisk A/S New compounds, their preparation and use
US6492406B1 (en) * 1999-05-21 2002-12-10 Astrazeneca Ab Pharmaceutically active compounds
EP1209158A1 (en) * 2000-11-18 2002-05-29 Aventis Pharma Deutschland GmbH Substituted beta-carbolines
WO2003039545A2 (en) * 2001-11-07 2003-05-15 Millennium Pharmaceuticals, Inc. Carboline derivatives as inhibitors of ikb in the treatment of multiple myeloma and others cancers
FR2869540B1 (en) * 2004-04-30 2008-05-16 Centre Nat Rech Scient Cnrse PHARMACEUTICAL COMPOSITIONS CONTAINING B-CARBOLINE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF CANCER
US8119655B2 (en) * 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
PT2137184E (en) * 2007-04-03 2013-08-01 Array Biopharma Inc Imidazo[1,2-a]pyridine compounds as receptor tyrosine kinase inhibitors
GB0723815D0 (en) * 2007-12-05 2008-01-16 Glaxo Group Ltd Compounds

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Publication number Publication date
TW201130833A (en) 2011-09-16
FR2953837B1 (en) 2012-03-09
FR2953837A1 (en) 2011-06-17
WO2011070298A1 (en) 2011-06-16
UY33099A (en) 2011-07-29

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